Catalog # |
Size |
Price |
|
---|---|---|---|
036-31 | 100 µg | $253 |
Gly-Gln-Lys-Gly-Gln-Val-Gly-Pro-Pro-Gly-Ala-Ala-Cys-Arg-Arg-Ala-Tyr-Ala-Ala-Phe-Ser-Val-Gly-NH2
|
2247.55 | |
| ≥ 95% |
| Exhibits correct molecular weight |
| Soluble in water |
|
Up to 6 months in lyophilized form at 0-5°C. For best results, rehydrate just before use. After rehydration, keep solution at +4°C for up to 5 days or freeze at -20°C for up to 3 months. Aliquot before freezing to avoid repeated freeze-thaw cycles. |
| White powder |
| Each vial contains 100 µg of NET peptide. |
G-protein-coupled receptors (GPCRs) represent an important group of targets for pharmaceutical therapeutics. The completion of the human genome revealed a large number of putative GPCRs. However, the identification of their natural ligands, and especially peptides, suffers from low discovery rates, thus impeding development of therapeutics based on these potential drug targets. We describe the discovery of novel GPCR ligands encrypted in the human proteome. Hundreds of potential peptide ligands were predicted by machine learning algorithms. In vitro screening of selected 33 peptides on a set of 152 GPCRs, including a group of designated orphan receptors, was conducted by intracellular calcium measurements and cAMP assays. The screening revealed eight novel peptides as potential agonists that specifically activated six different receptors in a dose-dependent manner. Most of the peptides showed distinct stimulatory patterns targeted at designated and orphan GPCRs. Further analysis demonstrated a significant in vivo effect for one of the peptides in a mouse inflammation model.
Shemesh R, Toporik A, Levine Z, et al. Discovery and validation of novel peptide agonists for G-protein-coupled receptors. J Biol Chem. 2008;283(50):34643-34649. doi:10.1074/jbc.M805181200
Abstract: Rationale: Relaxin is a hormone that has been considered as a potential therapy for patients with fibrotic diseases. Objectives: To gauge the potential efficacy of relaxin-based therapies in idiopathic pulmonary fibrosis (IPF), we studied gene expression for relaxin/insulin-like family peptide receptor 1 (RXFP1) in IPF lungs and controls. Methods: We analyzed gene expression data obtained from the Lung Tissue Research Consortium and correlated RXFP1 gene expression data with cross-sectional clinical and demographic data. We also employed ex vivo donor and IPF lung fibroblasts to test RXFP1 expression in vitro. We tested CGEN25009, a relaxin-like peptide, in lung fibroblasts and in bleomycin injury. Measurements and Main Results: We found that RXFP1 is significantly decreased in IPF. In patients with IPF, the magnitude of RXFP1 gene expression correlated directly with diffusing capacity of the lung for carbon monoxide (P < 0.0001). Significantly less RXFP1 was detected in vitro in IPF fibroblasts than in donor controls. Transforming growth factor-β decreased RXFP1 in both donor and IPF lung fibroblasts. CGEN25009 was effective at decreasing bleomycin-induced, acid-soluble collagen deposition in vivo. The relaxin-like actions of CGEN25009 were abrogated by RXFP1 silencing in vitro, and, in comparison with donor lung fibroblasts, IPF lung fibroblasts exhibited decreased sensitivity to the relaxin-like effects of CGEN25009. Conclusions: IPF is characterized by the loss of RXFP1 expression. RXFP1 expression is directly associated with pulmonary function in patients with IPF. The relaxin-like effects of CGEN25009 in vitro are dependent on expression of RXFP1. Our data suggest that patients with IPF with the highest RXFP1 expression would be predicted to be most sensitive to relaxin-based therapies.
Tan J, Tedrow JR, Dutta JA, et al. Expression of RXFP1 Is Decreased in Idiopathic Pulmonary Fibrosis. Implications for Relaxin-based Therapies. Am J Respir Crit Care Med. 2016;194(11):1392-1402. doi:10.1164/rccm.201509-1865OC
The relaxin-like RXFP1 ligand–receptor system has important functions in tumor growth and tissue invasion. Recently, we have identified the secreted protein, CTRP8, a member of the C1q/tumor necrosis factor-related protein (CTRP) family, as a novel ligand of the relaxin receptor, RXFP1, with functions in brain cancer. Here, we review the role of CTRP members in cancers cells with particular emphasis on CTRP8 in glioblastoma.
Thanasupawat T, Glogowska A, Burg M, et al. RXFP1 is Targeted by Complement C1q Tumor Necrosis Factor-Related Factor 8 in Brain Cancer. Front Endocrinol (Lausanne). 2015;6:127. Published 2015 Aug 13. doi:10.3389/fendo.2015.00127
No References
Catalog# | Product | Size | Price | Buy Now |
---|
Social Network Confirmation